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Radioactive labeled long-acting peptide targeted pharmaceutical and production method thereof

Inactive Publication Date: 2020-04-30
LI MING HSIN +9
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patent describes a new way to make a drug that can be used to diagnose and treat breast cancer. The drug is designed to attach to a protein in the blood, which helps to keep it in the blood for a longer time and reduces the chance of it getting trapped in normal tissues. This makes it easier to accurately diagnose and treat the cancer. The drug can also be combined with other medical imaging techniques to improve diagnosis and treatment, and reduce the cost of treating the cancer.

Problems solved by technology

However, the peptide pharmaceutical is good in water solubility, and the amount of tumor accumulation in the actual application is not as high as that of the protein pharmaceutical, and is rapidly metabolized in the body.
In the prior arts WO2016209795A1 and CN 104650217A, National Institutes of Health revealed the modified Evans Blue (EB) as the technology for the development of RGD-related pharmaceuticals, but it is also difficult to effectively overcome problem of radiation decay in storage and transport.

Method used

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  • Radioactive labeled long-acting peptide targeted pharmaceutical and production method thereof
  • Radioactive labeled long-acting peptide targeted pharmaceutical and production method thereof
  • Radioactive labeled long-acting peptide targeted pharmaceutical and production method thereof

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Embodiment Construction

[0023]The chemical structure of DOTA-EB-cRGDfK of the present invention is shown In FIG. 1, The radioactive labeled DOTA-EB-cRGDfK is prepared by adding 30 μg of DOTA-EB-cRGDfK peptide containing 20 μg / μL in DMSO solution, adding a radiation solution containing 111In or 68Ga or 177Lu), and adding 1M NaOAc solution to make the volume of 300 μL, the pH of the solution is 6-7 after mixing evenly. The radiation solution is placed in a 95° C. thermal reactor for 15 minutes and 1 μL was taken for ITLC analysis after cooling. The labeling efficiency showed greater than 90%. The radiation solution was taken for Radio-HPLC analysis at 20-30 μCi and the main signal showed a retention time of 7 minute.

[0024]Please refer to FIG. 2, which is a diagram showing the effect of concentration and pH of the radioactive labeled DOTA-EB-cRGDfK of the present invention, and FIG. 3, which shows the effect of radioactive labeled DOTA-EB-cRGDfK of the present invention, and the activity and concentration sta...

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Abstract

A radioactive labeled long-acting peptide-targeting pharmaceutical and production method, in which the peptide targeted pharmaceutical is firstly dissolved in a solution, followed by labeling the radioactive at a high temperature, and the dosage of the pharmaceutical with radioactive labeling is expected to be reduced and labeling efficiency is improved, and no further purification by filtration is required, which shortens the preparation process and reduces personnel exposure in the working environment. The radioactive labeled long-acting peptide-targeting pharmaceutical can increase the specific binding capacity of tumors and reduce the non-specific accumulation in normal tissues. It can be applied to the field of tumor and nuclear medicine for diagnosis and treatment of tumors and / or tumor metastases with efficacy and precision treatment.

Description

BACKGROUND OF THE INVENTION1. Field of the Invention[0001]The invention relates to a radioactive labeled long-acting targeted peptide pharmaceutical and a production method thereof, in particular to a targeted peptide pharmaceutical produced with improved labeling efficiency and minimum dosage required that reduces preparation time and cost.2. Description of Related Art[0002]According to the Global Cancer Report 2014 published by the World Health Organization (WHO), global cancer cases are growing rapidly from 14 million in 2012 to 19 million in 2025, and will reach 24 million by 2035. That is an increase of more than 70% in 23 years. At present, the development of targeted peptide pharmaceuticals has been a trend in decade. Tumor cells grow to 1-2 mm while migrate and grow due to their new blood vessels, and integrin acts as an influence on cell attachment, migration, growth and differentiation, and angiogenesis are highly expressed on inflammation and tumor endothelial cells, also...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61K51/04C07B59/00A61K49/00C07K7/64
CPCA61K51/088A61K2123/00A61K51/0482A61K49/0002C07B2200/05C07K7/64C07B59/008A61K49/0021A61K51/082C07B59/004C07K1/13
Inventor LI, MING-HSINCHANG, CHIH-HSIENCHEN, SU-JUNGLEE, SHIH-YINGLO, SHENG-NANCHEN, MING-WEIHUANG, YUAN-RUEIFENG, CHUN-FANGLO, SHIH-WEICHUANG, CHENG-HUI
Owner LI MING HSIN